|Systematic (IUPAC) name|
Galeterone (TOK-001 or VN/124-1) is a novel steroidal antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and an inhibitor of CYP17A1, an enzyme required for the biosynthesis of the androgens. It shows selectivity for 17,20-lyase over 17-hydroxylase. As of the second half of 2014, galeterone is in phase III clinical trials for castration-resistant prostate cancer.
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- Yin L, Hu Q (2014). "CYP17 inhibitors--abiraterone, C17,20-lyase inhibitors and multi-targeting agents". Nat Rev Urol 11 (1): 32–42. doi:10.1038/nrurol.2013.274. PMID 24276076.
- Yahoo! Finance (2014). "Tokai Pharmaceuticals’ Reformulated Galeterone Demonstrates Robust PSA Reductions in Advanced Prostate Cancer Patients".